ES2172882T3 - INTERMEDIATE PROCEDURES AND PRODUCTS FOR THE PREPARATION OF INDAZOL SUBSTITUTED DERIVATIVES. - Google Patents

INTERMEDIATE PROCEDURES AND PRODUCTS FOR THE PREPARATION OF INDAZOL SUBSTITUTED DERIVATIVES.

Info

Publication number
ES2172882T3
ES2172882T3 ES98913997T ES98913997T ES2172882T3 ES 2172882 T3 ES2172882 T3 ES 2172882T3 ES 98913997 T ES98913997 T ES 98913997T ES 98913997 T ES98913997 T ES 98913997T ES 2172882 T3 ES2172882 T3 ES 2172882T3
Authority
ES
Spain
Prior art keywords
alkyl
compound
preparation
indazol
optionally substituted
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
ES98913997T
Other languages
Spanish (es)
Inventor
Stephane Caron
Shane Allen Eisenbeis
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pfizer Products Inc
Original Assignee
Pfizer Products Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pfizer Products Inc filed Critical Pfizer Products Inc
Application granted granted Critical
Publication of ES2172882T3 publication Critical patent/ES2172882T3/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

Un procedimiento para la preparación de un compuesto de fórmula o una sal farmaceúticamente aceptable de dicho compuesto, en la que: R es alquilo (C1-C10) o -(CH2)n(fenilo), en el que n es un número entero que va de 0 a 2, y en el que dichos grupos R están opcionalmente sustituidos con 1 a 3 sustituyentes independientemente seleccionados entre cloro, fluoro, alcoxi (C1-C6) y trifluorometilo; R1 es alquilo (C1-C10), alquenilo (C2-C6) o fenilo, en el que dichos grupos R1 están opcionalmente sustituidos con 1 a 3 sustituyentes independientemente seleccionados entre trifluorometilo, cloro y fluoro; R2 es H, -C(Y)R4, -C(O)OR4, -C(Y)NR5R4, - C(Y)NR5OR4, o CN; R3 es H, alquilo (C1-C6) opcionalmente sustituido con hidroxi, -OR4, -CN, -C(Y)R4, -C(O)OR4, -C(Y)NR4R5, - C(Y)NR4OR5, -NR4OR5 o NR4R5; o R2 y R3 se unen formando =O; cada R4 y R5 es independientemente H o alquilo (C1- C6); y cada Y es independientemente O o S; el cual comprende el tratamiento de un compuesto de fórmula o una sal de dicho compuesto, en la que R, R1, R2 y R3 son lo definido anteriormente, con un ácido de Lewis y cianuro de tri-(aril C6-C10)sililo o cianuro de tri- (alquil C1-C6)sililo.A process for the preparation of a compound of the formula or a pharmaceutically acceptable salt of said compound, wherein: R is (C1-C10) alkyl or - (CH2) n (phenyl), in which n is an integer that ranges from 0 to 2, and wherein said R groups are optionally substituted with 1 to 3 substituents independently selected from chloro, fluoro, (C1-C6) alkoxy and trifluoromethyl; R1 is (C1-C10) alkyl, (C2-C6) alkenyl or phenyl, wherein said R1 groups are optionally substituted with 1 to 3 substituents independently selected from trifluoromethyl, chlorine and fluoro; R2 is H, -C (Y) R4, -C (O) OR4, -C (Y) NR5R4, -C (Y) NR5OR4, or CN; R3 is H, (C1-C6) alkyl optionally substituted with hydroxy, -OR4, -CN, -C (Y) R4, -C (O) OR4, -C (Y) NR4R5, - C (Y) NR4OR5, - NR4OR5 or NR4R5; or R2 and R3 join forming = O; each R4 and R5 is independently H or (C1-C6) alkyl; and each Y is independently O or S; which comprises the treatment of a compound of the formula or a salt of said compound, wherein R, R1, R2 and R3 are as defined above, with a Lewis acid and tri- (aryl C6-C10) silyl cyanide or tri- (C1-C6 alkyl) silyl cyanide.

ES98913997T 1997-05-08 1998-04-28 INTERMEDIATE PROCEDURES AND PRODUCTS FOR THE PREPARATION OF INDAZOL SUBSTITUTED DERIVATIVES. Expired - Lifetime ES2172882T3 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US4685897P 1997-05-08 1997-05-08

Publications (1)

Publication Number Publication Date
ES2172882T3 true ES2172882T3 (en) 2002-10-01

Family

ID=21945777

Family Applications (1)

Application Number Title Priority Date Filing Date
ES98913997T Expired - Lifetime ES2172882T3 (en) 1997-05-08 1998-04-28 INTERMEDIATE PROCEDURES AND PRODUCTS FOR THE PREPARATION OF INDAZOL SUBSTITUTED DERIVATIVES.

Country Status (12)

Country Link
US (1) US6011159A (en)
EP (1) EP0983249B1 (en)
JP (1) JP3399546B2 (en)
AR (2) AR015648A1 (en)
AT (1) ATE214373T1 (en)
AU (1) AU6849798A (en)
DE (1) DE69804212T2 (en)
DK (1) DK0983249T3 (en)
ES (1) ES2172882T3 (en)
PT (1) PT983249E (en)
WO (1) WO1998050367A1 (en)
ZA (1) ZA983842B (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AP1147A (en) * 1996-05-03 2003-02-25 Pfizer Substituted indazole derivatives and related compounds.
US6716978B2 (en) * 1997-11-04 2004-04-06 Pfizer Inc Therapeutically active compounds based on indazole bioisostere replacement of catechol in PDE4 inhibitors
JP2000198734A (en) * 1998-12-30 2000-07-18 Pfizer Inc Prokinetic agent for treating gastric hypomotility and related disease
KR100423899B1 (en) * 2000-05-10 2004-03-24 주식회사 엘지생명과학 Indazoles substituted with 1,1-dioxoisothiazolidine useful as inhibitors of cell proliferation
DE102004005172A1 (en) * 2004-02-02 2005-08-18 Aventis Pharma Deutschland Gmbh Indazole derivatives as inhibitors of the hormone sensitive lipase
US7459469B2 (en) 2004-11-10 2008-12-02 Targacept, Inc. Hydroxybenzoate salts of metanicotine compounds
UA88792C2 (en) * 2004-11-10 2009-11-25 Таргасепт, Інк. Hydroxybenzoate salts of metanicotine compounds
EP2357174A1 (en) 2006-05-09 2011-08-17 AstraZeneca AB Salt forms of (2S)-(4E)-N-Methyl-5-[(5-Isopropoxy)pyridin-3-yl]-4-penten-2-amine
TWI389889B (en) 2006-05-09 2013-03-21 Targacept Inc Novel polymorph forms of (2s)-(4e)-n-methyl-5-[3-(5-isopropoxypyridin)yl]-4-penten-2-amine

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU702105B2 (en) * 1994-10-20 1999-02-11 Pfizer Inc. Bicyclic tetrahydro pyrazolopyridines and their use as medicaments
AP1147A (en) * 1996-05-03 2003-02-25 Pfizer Substituted indazole derivatives and related compounds.

Also Published As

Publication number Publication date
AU6849798A (en) 1998-11-27
US6011159A (en) 2000-01-04
JP2000513019A (en) 2000-10-03
AR015648A1 (en) 2001-05-16
ZA983842B (en) 1999-11-08
EP0983249B1 (en) 2002-03-13
PT983249E (en) 2002-08-30
EP0983249A1 (en) 2000-03-08
JP3399546B2 (en) 2003-04-21
DE69804212T2 (en) 2002-07-25
DE69804212D1 (en) 2002-04-18
AR016737A1 (en) 2001-07-25
DK0983249T3 (en) 2002-07-08
WO1998050367A1 (en) 1998-11-12
ATE214373T1 (en) 2002-03-15

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